Antitargets
Prediction and Prevention of Drug Side Effects
(Sprache: Englisch)
This practice-oriented handbook surveys current knowledge on the prediction and prevention of adverse drug reactions related to off-target activity of small molecule drugs. It is unique in collating the current approaches into a single source, and includes...
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Klappentext zu „Antitargets “
This practice-oriented handbook surveys current knowledge on the prediction and prevention of adverse drug reactions related to off-target activity of small molecule drugs. It is unique in collating the current approaches into a single source, and includes several highly instructive case studies that may be used as guidelines on how to improve drug development projects.With its large section on ADME-related effects, this is key knowledge for every drug developer.
Inhaltsverzeichnis zu „Antitargets “
PART I: GENERAL ASPECTS- Why drugs fail: study on side effects in New Chemical Entities
- Predicting ADME properties and side effects: the BioPrint approach
PART II: ANTITARGETS AND SIDE-EFFECTS
- The hERG channel: biology and mutational information
- Pharmacophore for drugs involved in hERG blockage
- Pharmacological and regulatory aspects of prolonged QT
- Pharmacophore modeling for alpha1 receptors
PART III: ANTITARGETS IN ADME
- Cytochrome P450s: drug-drug interactions
- Cytochrome P450: an integrative modeling approach
- Cytochrome P450: common substructures and reactivity
- MetaSite: understanding metabolism in human cytochromes
- CyP induction by pregnane X receptor
- Ligand features essential for Cyp induction
- Transporters and drug discovery
- P-glycoprotein: computational models for substrates and inhibitors
PART IV: CASE STUDIES OF DRUG OPTIMIZATION AGAINST ANTITARGETS
- Januvia (Sitagliptin): a selective DPP4 inhibitor
- Optimization of hERG in drug discovery programs
- PRX-00023: a selective 5-HT1A agonist
Autoren-Porträt
Roy Vaz is the head of investigative pharmacokinetics at the Bridgewater, NJ (USA) location of Sanofi-Aventis Pharmaceuticals. He received his Ph.D. in Organic Chemistry from the University of Florida, Gainesville (USA), after graduating from the Indian Institute of Technology in Mumbai (India). Prior to his present appointment, he has worked with Bristol-Myers-Squibb and Tripos. He is a specialist on the prediction and modeling of cytochrome-mediated drug metabolism.Thomas Klabunde obtained his PhD in chemistry from the University of Mnster (Germany). After a postdoctoral fellowship at the Texas A&M University, he was appointed Assistant Professor at the Institute for Bioscience and Technology in Houston (USA). Later on, he joined the pharmaceutical research of Sanofi-Aventis in Frankfurt (Germany), where he is currently a group leader. His main interest lies with drug design approaches for G protein-coupled receptors, notably in the areas of lead finding and chemogenomics.
Bibliographische Angaben
- 2008, XXIV, 480 Seiten, 41 farbige Abbildungen, 58 Schwarz-Weiß-Abbildungen, Maße: 17,8 x 24,6 cm, Gebunden, Englisch
- Herausgegeben: Roy J. Vaz, Thomas Klabunde, Raimund Mannhold
- Verlag: Wiley-VCH
- ISBN-10: 3527318216
- ISBN-13: 9783527318216
- Erscheinungsdatum: 23.01.2008
Sprache:
Englisch
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